Medicine and Health Sciences Commons^™

Method For Designing Compounds And Compositions Useful For Targeting High Stoichiometric Complexes To Treat Conditions, Including Treatment Of Viruses, Bacteria, And Cancers Having Acquired Drug Resistance, Peixuan Guo, Dan Shu

Pharmaceutical Sciences Faculty Patents

A method is described for the identification o f multi-subunit biocomplex drug targets. The method includes identifying a target that performs a biological function, wherein the target comprises one or more subunits, wherein a minimum number of the one or more subunits is inactivated to inhibit the biological function. The method includes selecting a drug that binds specifically to each subunit of the one or more subunits with a target probability. The method describes a relationship between inhibition efficiency of the drug and total number of the one or more subunits using a binomial distribution, wherein the inhibition efficiency comprises …

Rna Nanoparticles And Method Of Use Thereof, Peixuan Guo, Hui Li, Wei Luo

Pharmaceutical Sciences Faculty Patents

The presently-disclosed subject matter relates to an artificial RNA nanostructure and method of use thereof. In particular, the presently-disclosed subject matter relates to RNA nanoparticles and RNA dendrimers, and methods of disease diagnosis and treatments using the RNA nanostructure and RNA dendrimers.

Rna Nanoparticle For Treatment Of Gastric Cancer, Peixuan Guo, Daxiang Cui, Dan Shu, Yi Shu, Chunlei Zhang

Pharmaceutical Sciences Faculty Patents

The presently-disclosed subject matter relates to RNA-based composition and method to treat gastric cancer in a subject. More particularly, the presently disclosed subject matter relates to a RNA nanostructure and composition containing a multiple branched RNA nanoparticle, a gastric cancer targeting module, and an effective amount of a therapeutic agent. Further, the presently disclosed subject matter relates to a method of using the RNA nanoparticle composition to treat gastric cancer in a subject having or at risk of having gastric cancer.

Cocaine Hydrolase-Fc Fusion Proteins For Cocaine And Methods For Utilizing The Same, Chang-Guo Zhan, Fang Zheng, Hsin-Hsiung Tai, Xiabin Chen, Liu Xue, Shurong Hou

Pharmaceutical Sciences Faculty Patents

The presently-disclosed subject matter includes isolated polypeptides that comprise a butyrylcholinestrase (BChE) polypeptide and a second polypeptide. The BChE polypeptide as well as the second polypeptide can be variants and/or fragments thereof. The presently-disclosed subject matter also includes a pharmaceutical composition that comprises the present isolated polypeptide and a suitable pharmaceutical carrier. Further still, methods are provided for treating cocaine-induced conditions, and comprise administering the isolated polypeptide and/or pharmaceutical compositions thereof to an individual.

Method And System For Terpene Production Platforms In Yeast, Joseph Chappell, Xun Zhuang, Shuiqin Wu

Pharmaceutical Sciences Faculty Patents

A method is provided for producing modified mutant yeast and the resulting yeast that can be used as a platform for terpene production. The method includes chemical mutagenesis to effect ergosterol dependent growth in yeast. Subsequently, these yeast are subjected to an erg9 knockout mutation to thereby produce ergosterol dependent growth/ erg9 knockout mutation yeast cell lines. The resulting yeast are well suited for use in the production of terpenes.

Vesicular Monoamine Transporter-2 Ligands And Their Use In The Treatment Of Psychostimulant Abuse, Linda P. Dwoskin, Peter Anthony Crooks, Guangrong Zheng, Justin Robert Nickell, Zheng Cao, Na-Ra Lee

Pharmaceutical Sciences Faculty Patents

The present invention relates to methods of treatment of a disease or pathology of the central nervous system, an eating disorder, or substance use disorder, drug dependence/abuse and withdrawal therefrom comprising administering at least one N-phenylalkyl amphetamine derivative and pharmaceutical compositions comprising at least one N-phenylalkyl amphetamine derivative to an individual in need thereof.

Lipid Bilayer-Integrated Spp1 Connector Protein Nanopore And Spp1 Connector Protein Variants For Use As Lipid Bilayer-Integrated Nanopore, Peixuan Guo, Shaoying Wang

Pharmaceutical Sciences Faculty Patents

A conductive channel-containing membrane includes a membrane layer, and a SPPl connector polypeptide variant that is incorporated into the membrane layer to form an aperture through which conductance can occur when an electrical potential is applied across the membrane. A method of sensing a molecule, such as a polypeptide or nucleic acid molecule, makes use of the conductive channel- containing membrane. A method of DNA sequence makes use of the conductive channel-containing membrane.

Method And System For Diterpene Production Platforms In Yeast, Joseph Chappell, Xun Zhuang, Shuiqin Wu

Pharmaceutical Sciences Faculty Patents

A method is provided for modifying yeast to express mutant avian farnesyl disphospate synthase and the resulting modified yeast. The yeast advantageously includes additional mutants including but not limited to having ergosterol dependent growth and being erg-. The modified yeast are beneficial for the production of various terpenes including diterpenes.

Rna Nanoparticles For Brain Tumor Treatment, Peixuan Guo, Carlo M. Croce, Tae Jin Lee, Farzin Haque, Hui Li

Pharmaceutical Sciences Faculty Patents

The presently-disclosed subject matter relates to an artificial RNA nanostructure molecule and method to treat brain tumor in a subject. More particularly, the presently disclosed subject matter relates to a RNA nanostructure containing a multiple branched RNA nanoparticle, a brain tumor targeting module, and an effective amount of a therapeutic agent. Further, the presently disclosed subject matter relates to a method of using the RNA nanostructure composition to treat brain tumor in a subject having or at risk of having brain tumor.

Identification Of Ebsulfur Analogues With Broad-Spectrum Antifungal Activity, Sylvie Garneau-Tsodikova, Huy X. Ngo, Sanjib K. Shrestha

Pharmaceutical Sciences Faculty Patents

The invention relates to novel ebsulfur analogues and novel pharmaceutical compositions comprising ebsulfur analogues. The invention also relates to novel methods of treating infections caused by fungal species comprising administration of ebselen, ebsulfur, and ebsulfur analogues.

Image Anaysis For Predicting Body Weight In Humans, Jeffrey S. Barrett, Chee Ng

Pharmaceutical Sciences Faculty Patents

Systems and methods for determining body weight predictions and human conditions are disclosed. A body weight may be predicted by capturing at least one image of a human, and determining, from the image, a body weight prediction of the human by processing the at least one image with a data processor. The body weight prediction may further be based on an age-based weight factor. A model such as a neural network model may be used to predict body weight.

Rna-Based Compositions And Adjuvants For Prophylactic And Therapeutic Treatment, Peixuan Guo, Hui Li, Emil F. Khisamutdinov, Daniel L. Jasinski

Pharmaceutical Sciences Faculty Patents

The present invention is directed towards an artificial RNA nano structure comprising multiple external strands of RNA, each external strand comprising about 40-50 nucleotides; one internal strand of RNA comprising more than about 50 nucleotides; the internal strands and external strands assembled to form a triangle nanostructure, a square nanostructure, or a polygon nanostructure and a pRNA three-way junction (3WJ) motif at each vertex of the nanostructure. Such nanostructure can be provided in a composition together with an adjuvant for use in inducing the production of high affinity neutralizing antibodies or inhibitory antibodies, inducing the production of cytokines, inducing an …

Compositions And Methods Of Modulating 15-Pgdh Activity, Sanford Markowitz, James K. Willson V, Bruce Posner, Joseph Ready, Youngyou Zhang, Hsin-Hsiung Tai, Monika Antezak, Stanton Gerson, Kibeom Bae, Sung Yeun Yang, Amar Desai

Pharmaceutical Sciences Faculty Patents

Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

Eis Inhibitors, Sylvie Garneau-Tsodikova, Oleg V. Tsodikov

Pharmaceutical Sciences Faculty Patents

Compounds and compositions are disclosed, which are useful as inhibitors of acetyltransferase Eis, a mediator of kanamycin resistance in Mycobacterium tuberculosis.

Eis Inhibitors, Sylvie Garneau-Tsodikova, Oleg V. Tsodikov, James E. Posey

Pharmaceutical Sciences Faculty Patents

Provided herein are novel small-molecules that have use in the inhibition of Eis, which mediates kanamycin resistance in Mycobacterium tuberculosis. The presently-disclosed subject matter further includes a pharmaceutical composition including a small molecule inhibitor, as described herein, and a suitable pharmaceutical carrier. Methods of treating tuberculosis comprising administering to an individual an effective amount of the disclosed small molecule inhibitors to mediate kanamycin A resistance and treat tuberculosis are also provided.

Cytochrome P450s And Uses Thereof, Joseph Chappell, Lyle F. Ralston

Pharmaceutical Sciences Faculty Patents

The invention relates to isolated cytochrome P450 polypeptides and nucleic acid molecules, as well as expression vectors and transgenic plants containing these molecules. In addition, the invention relates to uses of such molecules in methods of increasing the level of resistance against a disease caused by a plant pathogen in a transgenic plant, in methods for producing altered compounds, for example, hydroxylated compounds, and in methods of producing isoprenoid compounds.

Cytochrome P450s And Uses Thereof, Joseph Chappell, Lyle F. Ralston

Pharmaceutical Sciences Faculty Patents

The invention relates to isolated cytochrome P450 polypeptides and nucleic acid molecules, as well as expression vectors and transgenic plants containing these molecules. In addition, the invention relates to uses of such molecules in methods of increasing the level of resistance against a disease caused by a plant pathogen in a transgenic plant, in methods for producing altered compounds, for example, hydroxylated compounds, and in methods of producing isoprenoid compounds.

Bishydrazone-Based Antifungal Agents, Sylvie Garneau-Tsodikova, David S. Watt

Pharmaceutical Sciences Faculty Patents

Hydrazone compounds and pharmaceutical compositions including same are disclosed as having antifungal activity. Such compounds are useful for treating or preventing fungal conditions in a subject in need thereof by administering same.

Mutants Of Cocaine Esterase, Donald Landry, Chang-Guo Zhan

Pharmaceutical Sciences Faculty Patents

Provided are mutant cocaine esterase polypeptides and PEGylated formulations thereof.

Methods For Treating Neuropathic Pain, Joseph R. Holtman, Peter Anthony Crooks, Linda Phyliss Dwoskin, Michael J. Mcintosh, Elzbieta Pogonowska Wala

Pharmaceutical Sciences Faculty Patents

Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.

Static Multiple-Sample Nmr Probe, Eric Jon Munson, Matthew Jon Nethercott

Pharmaceutical Sciences Faculty Patents

A static solid-state nuclear magnetic resonance (NMR) probe includes multiple probe subunits each configured for holding a sample. Each probe subunit includes at least an associated magic angle spinning (MAS) module, a radio-frequency (RF) coil and an RF transmission line together defining an RF circuit. Each of the multiple probe subunits is individually held in a conducting housing isolating the RF circuit of the each of the probe subunit from any other of the plurality of probe subunits. The static solid-state NMR probe may include four or more probe subunits including four or more MAS modules.

Halogenated Diarylacetylenes And Methods Of Treating Cancer, Vitaliy M. Sviripa, Wen Zhang, Chunming Liu, David S. Watt

Pharmaceutical Sciences Faculty Patents

Halogenated diarylacetylenes, e.g., diarylacetylenes having at least one halo substituent in one aryl ring and an amine in the opposing aryl ring, can inhibit the proliferation of LSI 74T colon cancer cells through the inhibition of c-myc and induction of the cyclin-dependent kinase inhibitor-I (i.e., p21(Wifl/Cipl)). Such compounds are useful as antineoplastic agents.

High Activity Mutants Of Cocaine Esterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Lei Fang

Pharmaceutical Sciences Faculty Patents

The Bacterial cocaine esterase (CocE) mutants disclosed herein each have enhanced catalytic efficiency for ( -)cocaine, as compared to CocE mutants in the prior art, including CocE mutant E172-173. The presently-disclosed subject matter further includes a pharmaceutical composition including a mutant of bacterial cocaine hydrolase, as described herein, and a suitable pharmaceutical carrier. The presently-disclosed subject matter further includes a method of treating a cocaine-induced condition comprising administering to an individual an effective amount of a mutant of bacterial cocaine hydrolase variant, as disclosed herein, to accelerate cocaine metabolism and produce biologically inactive metabolites.

Synthesis Of Non-Natural Cofactor Analogs Of S-Adenosyl-L-Methionine Using Methionine Adenosyltransferase, Jon S. Thorson, Tyler Huber, Jianjun Zhang, Shanteri Singh

Pharmaceutical Sciences Faculty Patents

The present disclosure relates to the synthesis of non-natural analogs of S-adenosyl-L-methionine (SAM) and/or of Se-adenosyl- L-methionine (SeAM) by reacting a methionine analog and adenosine triphosphate (ATP) in the presence of at least one methionine adenosyltransferase (MAT), and to use thereof with downstream SAM and/or SeAM utilizing enzymes.

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Compositions And Methods Of Modulating 15-Pgdh Activity, Sanford Markowitz, James K. V. Willson, Bruce A. Posner, Joseph Ready, Yongyou Zhang, Hsin-Hsiung Tai, Monika Antczak, Stanton Gerson, Kibeom Bae, Sung Yeun Yang, Amar Desai

Pharmaceutical Sciences Faculty Patents

Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

Bis-Quaternary Ammonium Cyclophane Compounds That Interact With Neuronal Nicotinic Acetylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, David Allen, Zhenfa Zheng, Paul Lockman

Pharmaceutical Sciences Faculty Patents

Provided are bis-quaternary ammonium cyclophane compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.

Selective Immunoproteasome Inhibitors With Non-Peptide Scaffolds, Chang-Guo Zhan, Kyung Bo Kim, Vinod Kasam, Na-Re Lee

Pharmaceutical Sciences Faculty Patents

Compounds useful for inhibiting the immunoproteasome have the formula of [image on patent].

Methods and compounds for inhibiting the immunoproteasome, particularly, immunoproteasome inhibitors with non-peptide scaffolds, are described.

Compounds Including Cox Inhibitor Moiety And Enhanced Delivery Of Active Drugs Using Same, Audra Stinchcomb, Kyung Bo Kim, Ragotham Reddy Pinninti, Priyanka Ghosh, Kalpana S. Paudel

Pharmaceutical Sciences Faculty Patents

The presently-disclosed subject matter includes compounds including a cyclooxygenase enzyme inhibitor moiety and a moiety derived from a drug of interest. In some embodiments, the drug of interest is an opioid. In some embodiments, the compound includes a diclofenac moiety and a naltrexone or naltrexol moiety. The compounds allow for enhanced delivery rates across skin.

Mono Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Zhenfa Zheng

Pharmaceutical Sciences Faculty Patents

Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and gastrointestinal tract disorders.

Bis-Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran

Pharmaceutical Sciences Faculty Patents

Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.